Composition for deterring the desire for tobacco



United States Patet O COMPOSITION FOR DETERRING THE DESIRE FOR TOBACCO Gustav W. Rapp, Glen Ellyn, IlL, assignor, by mesne assignments, to Reuslow P. Sherer, Ralph E. Kraefscli,

as trustees This invention relates to compositions for use in curbing the tobacco habit and it relates more particularly to a composition which may be taken orally, as in the form of a pill, tablet, capsule, chewing gum, or the like for use in deterring the desire for tobacco in such forms as cigarettes, cigars, smoking pipe tobacco, cheW- ing tobacco and the like. a

This application is a consolidation of the subject matter described and claimed and may therefore be considered to be a continuation-in-part of my copending applications Ser. No. 130,853, filed December 2, 1949, now abandoned, Ser. No. 137,280, filed January 6, 1950, now abandoned, and Ser. No. 269,337, filed lanuary 31, 1952 now abandoned, as a continuation-in-part of application Ser. No. 126,687, filed November 10, 1949, now abandoned.

As described in the aforementioned copending applications, there are many instances Where by desire or by necessity a person Wishes to dispense with the tobacco habit, yet finds it difficult to abstain, especially during the initial periods of restraint. Often times the desire to give up the tobacco habit arises out of personal preference but more often it arises out of necessity for medical purposes. Various investigations have been conducted to determine the effect of smoking on the health and intelligence of the public. For example, one of the more recent investigations has established the increased incidence in cancer which results from smoking and the like use of tobacco.

As a result it has been desirable and it is an object of this invention to provide means by which ones desire for tobacco may be effectively curbed, preferably by means of a composition which can be taken safely to satisfy ones desire for tobacco in its various forms so that abstinence will become easier or the use of tobacco entirely eliminated. It is particularly desirable to make use of a composition which is free of harmful ingredicuts and which may be taken orally, as in the form of pills, capsules, lozenges, chewing gum and the like without harmful effect and without undesirable reactions to the human system, and it is an object of this invention to produce a composition embodying such characteristics.

In accordance with this invention it has been found that lobeline, when made available in the human system, offers a physiological saturation which tends to curb the desire for tobacco in any one of the various ways in which such tobacco products are used by the human. The lobeline compound can be made available to give the desired results by oral administration of substances containing substantially water soluble salts of lobeline. The preferred water soluble salt of lobeline is lobelme sulphate but other salts such as the corresponding chlorides, phosphates, nitrates or organic salts of acetate, formate, oxalate, citrate and the like may also be used. Calculated on the basis of lobeline sulphate, best results have been secured when taken in dosages ranging from 1-8 mg. although it will be understood that more or less may be used to give corresponding results.

Attempts have been made in the past to make use of lobeline sulphate for curbing the desire for tobacco but the physiological effects which accompanied their use have caused more harm and became more undesirable than the continuance of the tobacco habit and such attempts have therefore resulted in failure. Wright and Littauer, Journal of American Medical Society, volume 109, pages 649-654, found that it was necessary to make use of lobeline sulphate in dosages as high as 8 mg. before any effect was secured on the tobacco habit but that when used in such dosages, the nausea, stomach upset and other undesirable physiological effects which accompanied the administration of such amounts of lobeline sulphate were more than the patient could stand. When the dosages of lobeline sulphate were reduced to 4 mg. for the purpose of minimizing these undesirable physiological side effects, no desirable effect was available for curbing the tobacco habit. This approach for the solution of the problem was therefore abandoned.

It has now been found that successful use can be made of lobeline sulphate or other of the soluble lobeline compounds to curb or eliminate the desire for tobacco without experiencing the undesirable side effects of nausea, stomach upset and the like, if the lobeline sulphate is administered in combination with an antacid compound that is capable of ionization in the environment to which it is subjected upon oral administration. It has been found further that the combination of lobeline salts with an antacid for oral administration is effective to curb the desire for tobacco when the lobeline compound is present in amounts considerably less than that which formed the lower limit in the unsuccessful formulations of Wright and Littauer. For example, good results have been secured with dosages containing as little as 1 mg. of lobeline sulphate. Dosages containing as much as 8 mg. of lobeline sulphate in combination with antacids have been used without undesirable physiological side effects and the higher dosages have provided considerably greater effect on the tobacco habit than would have been available from equivalent dosages of lobeline sulphate without the antacid. These synergistic effects eliminate the undersirable physiological side effects heretofore experienced in the use of lobeline sulphate and increase the activity of the lobeline sulphate for the purpose for which it is intended so that greater effect can be had with larger amounts and successful use can be made of amounts which have heretofore been incapable of giving the desired results. Most effective use of these substances is made when the lobeline compound is present in the ratio of l-8 parts by weight lobeline sulphate or other lobeline salts to about 100 parts by Weight of the antacid. It will the variable characteristics of the human beings.

Suitable antacids are represented by compounds capable of developing the alkaline reactions upon ionization when administered orally to the human being. These include such materials as the salts of weak acids and strong bases, such as the metal carbonates, including magnesium carbonate, calcium carbonate, sodium bicarbonate, potassium bicarbonate, or phosphates such as magnesium phosphate, aluminum phosphate, sodium hydrogen phosphate, tricalcium phosphate and the like, or metal silicates such as aluminum trisilicate, aluminum glycinate and the like, or hydroxides such as calcium hydroxide, magnesium hydroxide, aluminum hydroxide, sodium or potassium hydroxide and the like. Excellent use is made of an antacid composition which is almost immediately effective upon oral administration but it is preferred to make use of an immediately effective antacid (rapid acting antacid) in combination with another antacid which is slower acting (slow acting antacid) to be effective over a longer period of time.

The term rapid acting antacid, often referred to in the trade as systemic antacids, is intended to include such antacids as magnesium carbonate, calcium carbonate, tricalcium phosphate, tribasic magnesium phosphate, sodium bicarbonate, potassium bicarbonate, sodium hydroxide, potassium hydroxide and the like compounds. The term slow acting antacid or non-systemic antacids is meant to include such compounds as aluminum phosphate, magnesium silicate, magnesium phosphate, calcium phosphate, aluminum trisilicate, aluminum hydroxide and the like antacids. The combination of magnesium carbonate and aluminum hydroxide or of magnesium carbonate and tricalcium phosphate are representative of the preferred combinations of a. rapid acting and a slow acting antacid used with lobeline sulphate.

Instead of magnesium carbonate, use may be made of calcium carbonate, sodium bicarbonate, or sodium hydroxide. Instead of aluminum hydroxide, use may be made of such materials as aluminum phosphate, magnesium phosphate, aluminum trisilicate, tricalcium phosphate and the like.

To make the compositions more palatable, various flavoring substances well known in the food art may be added in sufiicient quantity to be effective. For example, traces of oils such as peppermint oil, oil of Wintergreen, cinnamon oil and the like may be used. In the selection of flavorings such materials as peppermint oil are preferred because it is effective in helping to overcome any tendency toward nausea. The dosages of lobeline sulphate in combination with the antacids may be formulated together into the desired pharmaceutical composition but the materials very often are combined with various fillers such as sucrose and the like in capsulating or in the manufacture of pills.

By way of illustration, but not by way of limitation, the following are examples of suitable compositions which may be used in the practice of this invention. The amounts set forth respond to effective dosages.

Example I l-8 milligrans lobeline sulphate 100 milligrams magnesium carbonate Trace peppermint oil Example ll 1-8 milligrams lobeline sulphate 40-60 milligrams magnesium carbonate 60-40 milligrams aluminum hydroxide Trace flavoring Example III 2 milligrams lobeline sulphate 50 milligrams magnesium carbonate 50 milligrams aluminum hydroxide Trace peppermint oil Example IV 2 milligrams lobeline nitrate 50 milligrams sodium bicarbonate 50 milligrams aluminum phosphate Example V 3 milligrams lobeline phosphate 50 milligrams aluminum phosphate 50 milligrams calcium carbonate Trace of oil of Wintergreen Example V1 2 milligrams lobeline sulphate 100 milligrams aluminum trisilicate Filler Example VII 4 milligrams lobeline sulphate 80 milligrams aluminum glycmate Filler Example VIII 5 milligrams lobeline sulphate 200 milligrams sodium bicarbonate Example 1X 1 milligram lobeline sulphate 100 milligrams aluminum trisilicate 100 milligrams magnesium carbonate Example X 3 milligrams lobeline sulphate 50 milligrams aluminum silicate 75 milligrams magnesium carbonate Example XI 2 milligrams lobeline sulphate 2 grains tricalcium' phosphate 2 grains magnesium carbonate Milk sugar filler Peppermint oil flavoring ministration of lobeline sulphate or its salts may be alleviated without loss in effect for curbing the desire for tobacco when the lobeline compound is kept from solution upon oral administration until it has passed through the stomach and into the intestinal region, and the desired results are available especially when such lobeline compounds are present in combination with antacids as previously described. These conditions for avoiding solubility until the compound has passed into the intestinal region have been achieved by enclosing the lobeline sulphate or other lobeline salt in an enteric coating formed of a material which has little, if any, solubility in the acidic fluids to which it is subjected during passage from the oral cavity to the intestinal region but which disintegrates or dissolves rather rapidly in the basic media in the intestinal tract to permit the lobeline to go into solution for the desired effect.

Example XII of an admixture of 1-8 mg. lobeline sulphate, mg. powdered sucrose.

The pill is immersed by suitable means in a thick aqueous solution of gelatin and the dipping operation may be repeated a number of times with interim setting until the desired thickness of gelatin has been built up as a continuous film about the pill or tablet. The coated pill or tablet is immersed in a 10 percent formaldehyde solution for about 5-10 seconds to harden the gelatin coating and render 1t insoluble to acidic aqueous medium. Example XIII A pill for a single dosage is formulated with 2 mg. lobeline sulphate, 50 mg. magnesium carbonate, and 50 mg. aluminum hydroxide. One or a number of pills so prepared are rolled in a solution of keratin dissolved in equal parts by volume of alcohol and ammonium hydroxide. The coated pills are allowed to set on a plate coated with olive oil or other fatty excipient. Instead of the keratin solution, a liquid composition of shellac dissolved in cetyl alcohol and acetone or shellac dissolved in castor oil and alcohol present in the ratio of 5 parts shellac and 1 part castor oil may be used to provide the protective coating.

Example XIV l.8 mg. lobeline sulphate are compounded with sufiicient lactose in finely divided form to provide a pill or capsule suitable for a single dosage (usually about mg. of lactose is sufficient).

Pills or tablets formed of the above composition are rolled in an enamelled pan with about one-half their weight phenyl salicylate which has been heated to melt temperature above The phenyl salicylate congeals as a continuous film about the pills. These coating operations may be repeated one or a number of times to build up the desired thickness calculated to prevent solution in the stomach.

Example XV Instead of the magnesium carbonate and aluminum hydroxide of Example XIII, the formulation to be enclosed within the enteric coating may be formulated of 2 mg. lobeline sulphate, 2 grains tricalcium phosphate and 2 grains magnesium carbonate with suitable fillers such as powdered sugar, milk sugar and the like, with or without a flavoring substance.

it will be understood that changes may be made in the details of formulation by substitution of equivalent materials in corresponding effective amounts and that the essential ingredients may be formulated into solutions for oral administration as a liquid instead of administration as a dry substance in the form of a pill, lozenge or the like, and that other changes may be made without departing from the spirit of the invention, especially as defined in the following claims.

I claim:

1. A medicinal preparation for use in the treatment and control of the tobacco habit comprising lobeline sulphate and aluminum hydroxide.

2. A medicinal preparation for use in the treatment and control of the tobacco habit comprising lobeline sulphate and an antacid selected from the group consisting of magnesium carbonate, calcium carbonate, sodium bicarbonate, potassium bicarbonate, magnesium phosphate,

aluminum phosphate, sodium hydrogen phosphate, tricalcium phosphate, aluminum silicate, aluminum glycinate, calcium hydroxide, magnesium hydroxide, aluminum hydroxide, sodium hydroxide, potassium hydroxide, and mixtures thereof.

medicinal preparation for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline and aluminum hydroxide.

4. A medicinal preparation for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline and magnesium carbonate.

A medicinal preparation for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline and sodium bicarbonate.

6. A medicinal preparation for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline and aluminum trisilicate. composition for use in the treatment and control obacco habit comprising a soluble salt of lobeline phosphate, sodium hydrogen phosphate, tricalcium phosphate, aluminum silicates, aluminum glycinate, calcium hydroxide, magnesium hydroxide, aluminum hydroxide, sodium hydroxide, potassium hydroxide, and mixtures thereof.

8. A composition as claimed in claim 7 in which, in a dosage for oral administration, the lobeline salt is present in amounts ranging from 1-8 milligrams.

composition as claimed in claim 7 in which the materials are present in amounts ranging from 1-8 parts by weight of the lobeline salt to 25-100 parts by weight of the antacid.

10. A composition for use of the tobacco habit comprising a soluble salt of lobeline and a combination of antacids consisting essentially of a systemic antacid and a non-systemic antacid.

composition as claimed in claim 10 in which the slow and rapi acting antacids are present in the ratio of 4060 parts by weight of the rapid acting antacid to 6040 parts by weight of the slow acting antacid.

dosage for use in the treatment and control of the tobacco habit comprising 1-8 milligrams of a soluble salt of lobeline, an antacid selected from the group consisting of magnesium carbonate, calcium carbonate, so-

in the treatment and control salt to 25-100 parts by weight of the antacid and in which the materials are contained within an enteric coating.

13. A composition for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline, a combination of. antacids, consisting essentially of a systemic antacid and a non-systemic antacid and in which the materials are contained With an enteric coating that is substantially insoluble in the acidic medium existing upon oral administration but which is soluble in the basic media of the intestinal tract.

14. A dosage for use in the treatment and control of the tobacco habit comprising 1-8 milligrams of a soluble salt of lobeline, aluminum hydroxide, and in which the materials are contained Within an enteric coating.

15. A dosage for use in the treatment and control of the tobacco habit comprising 1-8 milligrams of a soluble salt of lobeline, magnesium carbonate, and in which the materials are contained Within an enteric coating.

composition for use in the treatment and control of the tobacco habit comprising a soluble salt of lobeline, magnesium carbonate and tricalcium phosphate.

17. A dosage'for use in the treatment and control of the tobacco habit comprising 1-8 milligrams lobeline sulphate, magnesium carbonate and tricalcium phosphate, and in which the materials are contained within an enteric coating.

References Cited in the file of this patent Wright: Jour. of the Amer. Medical Assn, vol. 109, August 28, 1937, pp. 649 to 654. S. Dispensatory, 24th ed. (1947), pp. 54 to 56, 651, 2G 6utman: Modern Drug Encyclopedia, 2nd ed. (1941),

U. S. Dispensatory, 24th ed. (1947), p. 654. Merck Index, 6th ed. (1952), pp. 116, 118.

S. Dispensatory, 24th ed. 1947), p. 1187. New Modern Drugs, January 1948, p. 534. 

10. A COMPOSITION FOR USE IN THE TREATMENT AND CONTROL OF THE TOBACCO HABIT COMPRISING A SOLUBLE SALT OF LOBELINE AND A COMBINATION OF ANTACIDS CONSISTING ESSENTIALLY OF A SYSTEMIC ANTACID AND A NON-SYSTEMIC ANTACID. 